一系列N-烷基-1,4-二硫杂环己二烯的合成、体外抗菌和抗真菌活性

Syntheses, in vitro antibacterial and antifungal activities of a series of N-alkyl, 1,4-dithiines.

作者信息

Zentz F, Labia R, Sirot D, Faure O, Grillot R, Valla A

机构信息

Chimie et biologie des substances naturelles, FRE 2125 CNRS, 6, rue de l'Université, 29000 Quimper, France.

出版信息

Farmaco. 2005 Nov-Dec;60(11-12):944-7. doi: 10.1016/j.farmac.2005.06.015. Epub 2005 Oct 18.

DOI:10.1016/j.farmac.2005.06.015

Abstract

A series of dithiines were synthesized by cyclization of 4-(alkylamino)-4-oxobutanoic acids under the action of SOCl2. Their in vitro antibacterial and antifungal activities have been evaluated against reference strains and versus reference compounds. The so-called 'isoimides' 2a, 2b were totally inactive whereas some imides had low MICs for few bacteria and for few fungal microorganisms.

摘要

通过4-(烷基氨基)-4-氧代丁酸在SOCl₂作用下环化合成了一系列二硫代噻吩。已针对参考菌株并与参考化合物对比评估了它们的体外抗菌和抗真菌活性。所谓的“异酰亚胺”2a、2b完全无活性，而一些酰亚胺对少数细菌和少数真菌微生物具有较低的最低抑菌浓度。

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